Synthesis, Antimicrobial Activities and Molecular Docking Studies of Novel 6-Hydroxybenzofuran-3(2H)-one Based 2,4-Disubstituted 1,3-Thiazoles

被引：0

作者：

Laczkowski, Krzysztof Z. ^{[1
]}

Misiura, Konrad ^{[1
]}

Biernasiuk, Anna ^{[2
]}

Malm, Anna ^{[2
]}

Siwek, Agata ^{[3
]}

Plech, Tomasz ^{[3
]}

机构：

[1] Nicholas Copernicus Univ, Fac Pharm, Dept Chem Technol & Pharmaceut, Coll Med, PL-85089 Bydgoszcz, Poland

[2] Med Univ Lublin, Fac Pharm, Dept Pharmaceut Microbiol, PL-20093 Lublin, Poland

[3] Med Univ Lublin, Fac Pharm, Dept Organ Chem, PL-20093 Lublin, Poland

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2013年 / 10卷 / 09期

关键词：

Thiazoles; Thiosemicarbazones; Benzofuranone; Antimicrobial drugs; N-myristoyltransferase; Molecular modeling; FUNGAL N-MYRISTOYLTRANSFERASE; IN-VITRO ACTIVITY; ANTIFUNGAL AGENTS; CRYSTAL-STRUCTURE; CANDIDA-ALBICANS; 2-THIAZOLYLHYDRAZONE DERIVATIVES; BIOLOGICAL EVALUATION; ASYMMETRIC-SYNTHESIS; INHIBITORS; THIAZOLES;

D O I：

暂无

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis, characterization and investigation of antibacterial and antifungal activities of thirteen novel 6-hydroxybenzofuran-3(2H)-one based 2,4-disubstituted 1,3-thiazoles are presented. Their structures were determined using NMR, FAB MS and HRMS analyses. The results of microbiological screening reveal that three derivatives containing fluorine, bromine and hydrogen substituents at the phenyl ring are the most active antimicrobial compounds. Molecular docking studies of all compounds on the active sites of microbial enzymes indicated a possible target N-myristoyltransferase (NMT).

引用

页码：798 / 807

页数：10

共 50 条

[21] Synthesis and biological evaluation of novel 2-(1H-imidazol-2-ylmethylidene)hydrazinyl-1,3-thiazoles as potential antimicrobial agents
Laczkowski, Krzysztof Z.
Jachowicz, Katarzyna
Misiura, Konrad
Biernasiuk, Anna
Malm, Anna
HETEROCYCLIC COMMUNICATIONS, 2015, 21 (02) : 109 - 114
[22] Synthesis and Antibacterial Activity of Novel Fused 1,3-Thiazoles and 1,3-Thiazines Incorporating a 2,4-Dihydroxyphenyl Residue
Matysiak, Joanna
Los, Renata
Malm, Anna
Karpinska, Monika M.
Glaszcz, Urszula
Rajtar, Barbara
Polz-Dacewicz, Malgorzata
Wesolowska-Trojanowska, Marta
Niewiadomy, Andrzej
ARCHIV DER PHARMAZIE, 2012, 345 (04) : 302 - 313
[23] Synthesis of 2,4-disubstituted isoquinolin-1(2H)-ones based on reactions of α-substituted 2-lithio-β-methoxystyrenes with isocyanates
Kobayashi, Kazuhiro
Hayashi, Kazutaka
Nam, Changeng
Fukamachi, Shuhei
Konishi, Hisatoshi
HETEROCYCLES, 2008, 75 (05) : 1225 - 1231
[24] SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NOVEL 3, 6-DISUBSTITUTED IMIDAZO [2, 1-B] [1, 3] THIAZOLES
Rajurkar, V. G.
Patil, R. B.
Miniyar, P. B.
INTERNATIONAL JOURNAL OF PHARMACEUTICAL SCIENCES AND RESEARCH, 2011, 2 (06): : 1537 - 1542
[25] THE SYNTHESIS OF SOME 2,4-DISUBSTITUTED 6H-5,1,3-BENZOTHIADIAZOCINES
BODAJLA, M
STANKOVSKY, S
SPIRKOVA, K
COLLECTION OF CZECHOSLOVAK CHEMICAL COMMUNICATIONS, 1995, 60 (08) : 1415 - 1417
[26] PYRIDAZINONES .1. PREPARATION OF 2,4-DISUBSTITUTED 5-HYDROXY-3(2H)-PYRIDAZINONES AND 2,5-DISUBSTITUTED 4-HYDROXY-3(2H)-PYRIDAZINONES
KONECNY, V
CHEMICKE ZVESTI, 1976, 30 (05): : 663 - 673
[27] Design, Antimicrobial Testing, and Molecular Docking Studies of New Chalcone and Pyrimidine Derivatives based on 2-phenyl-1H-pyrazol-3(2H)-one
Alolayan, Ruba A.
Elkanzi, Nadia A. A.
Hrichi, Hajer
Dhafer, Cyrine El Baher
Zahou, Faten M.
Bakr, Rania B.
LETTERS IN DRUG DESIGN & DISCOVERY, 2024, 21 (10) : 1864 - 1873
[28] Synthesis and molecular docking studies of 5-acetyl-2-(arylidenehydrazin-1-yl)-4-methyl-1,3-thiazoles as α-amylase inhibitors
Mehmood, Hasnain
Haroon, Muhammad
Akhtar, Tashfeen
Woodward, Simon
Andleeb, Hina
JOURNAL OF MOLECULAR STRUCTURE, 2022, 1250
[29] Synthesis, Characterization, Anticancer and Antimicrobial Activity Studies of Novel Isomeric 2,4-Disubstituted Ureide Derivatives of Pyrimidinopiperidines
Bhavanam, Lourdu Rani
Kotra, Vijay
Mule, Sivanagi Reddy
Khandapu, Bala Murali Krishna
Bollikolla, Hari Babu
CHEMISTRYSELECT, 2019, 4 (01): : 441 - 450
[30] SYNTHESIS AND STRUCTURAL STUDY OF 2,4-DISUBSTITUTED 1,3-DIARYL-1,3,2,4-DIAZADIPHOSPHETIDINES
CHEN, HJ
HALTIWANGER, RC
HILL, TG
THOMPSON, ML
COONS, DE
NORMAN, AD
INORGANIC CHEMISTRY, 1985, 24 (26) : 4725 - 4730

← 1 2 3 4 5 →